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  2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. Org 27569

Org 27569 是有效的 CB1 receptor 變構(gòu)調(diào)節(jié)劑，既能增加激動(dòng)劑與 CB1 結(jié)合，又能抑制激動(dòng)劑誘導(dǎo)的 CB1 信號通路。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Org 27569 Chemical Structure

Org 27569 Chemical Structure

CAS No. : 868273-06-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥555
In-stock
1 mg ￥202
In-stock
5 mg ￥505
In-stock
10 mg ￥810
In-stock
50 mg ￥3464
In-stock
100 mg   詢價(jià)  
200 mg   詢價(jià)  

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查看 Cannabinoid Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
83 nM
Compound: 1; Org27569
Positive allosteric modulator activity at human CB1R expressed in CHO cells assessed as enhanced binding of [3H]CP55,940 after 60 mins by liquid scintillation spectrometric analysis
Positive allosteric modulator activity at human CB1R expressed in CHO cells assessed as enhanced binding of [3H]CP55,940 after 60 mins by liquid scintillation spectrometric analysis
[PMID: 26529344]
CHO-K1 IC50
2 nM
Compound: Org27569
Negative allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940 induced beta arrestin recruitment preincubated for 30 mins followed by addition of CP55940 for 90 mins by chemiluminescence assay
Negative allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940 induced beta arrestin recruitment preincubated for 30 mins followed by addition of CP55940 for 90 mins by chemiluminescence assay
[PMID: 27542310]
CHO-K1 EC50
324 nM
Compound: 1; Org27569
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte
[PMID: 26529344]
CHO-K1 EC50
9.05 nM
Compound: 1; Org27569
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay
Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay
[PMID: 26529344]
HEK293 EC50
0.64 μM
Compound: 1, ORG27569
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins in presence of CP55,940 by cAMP BRET assay
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins in presence of CP55,940 by cAMP BRET assay
[PMID: 26203658]
HEK293 EC50
10.59 μM
Compound: 1, ORG27569
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay
[PMID: 26203658]
HEK293 EC50
2.09 μM
Compound: 1, ORG27569
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 10 mins in presence of CP55,940 by cAMP BRET assay
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 10 mins in presence of CP55,940 by cAMP BRET assay
[PMID: 26203658]
HEK293 EC50
2.24 μM
Compound: 1, ORG27569
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay
Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay
[PMID: 26203658]
體外研究
(In Vitro)

Org 27569 增強(qiáng)激動(dòng)劑 (CP55940) 結(jié)合，促進(jìn)激動(dòng)劑與 CB1 的結(jié)合，但抑制激動(dòng)劑誘導(dǎo)的 G 蛋白激活并阻斷激動(dòng)劑誘導(dǎo)的 TM6 構(gòu)象變化。Org 27569 抑制激動(dòng)劑誘導(dǎo)的CB1 TM6運(yùn)動(dòng)，通過熒光探針在 342 位點(diǎn)檢測[2]。Org 27569 產(chǎn)生顯著但可飽和的特異性[3H]CP 55，940 結(jié)合水平增加。Org 27569 (1 μM) 抑制電誘發(fā)的小鼠輸精管收縮，pEC50 和 Emax 分別為 8.66±0.11 和 77% (95% 置信限，70.6 -82.7[4]。在 hCB1R 細(xì)胞中，Org 27569 (1 和 10 μM) 表現(xiàn)為弱逆激動(dòng)劑，產(chǎn)生少量但顯著的 [35S]GTPγS 結(jié)合降低。Org 27569 作為 WIN55212 介導(dǎo)的毛喉素刺激的 cAMP 產(chǎn)生抑制的抑制劑效果較差。Org 27569 誘導(dǎo) ERK1/2 磷酸化，Emax 為 19%，pEC50 值為 8.55±0.99[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

ORG 27569 (3.2 和 5.6 mg/kg，腹腔注射) 顯著減弱可卡因相關(guān)線索誘導(dǎo)的恢復(fù)、可卡因啟動(dòng)誘導(dǎo)的恢復(fù)、甲基苯丙胺相關(guān)線索誘導(dǎo)的恢復(fù)和甲基苯丙胺啟動(dòng)誘導(dǎo)的大鼠恢復(fù)[1]。Org27569 (30 mg/kg，ip) 產(chǎn)生獨(dú)立于 CB1 的食欲減退作用，并且不影響 anandamide (AEA) 的辨別刺激作用。與載體[3]相比，Org27569 (腦室內(nèi)注射 100 μg) 不影響全身給藥 CP55，940 的藥理作用。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

409.95

Formula

C24H28ClN3O
CAS 號
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 52.2 mg/mL (127.33 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.4393 mL 12.1966 mL 24.3932 mL
5 mM 0.4879 mL 2.4393 mL 4.8786 mL
查看完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.10 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.10 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.40%

參考文獻(xiàn)
Kinase Assay
[4]

Binding assays are performed with the CB1 receptor agonist [3H]CP 55,940 (0.7 nM) and the CB1 receptor antagonist [3H]SR 141716A (1.2 nM), 1 mg/mL BSA and 50 mM Tris buffer containing 0.1 mM EDTA and 0.5 mM MgCl2, pH 7.4, in a total assay volume of 500 μL. Binding is initiated by the addition of mouse brain membranes (30 μg). Assays are carried out at 37°C for 60 min before termination by addition of ice-cold wash buffer (50 mM Tris buffer and 1 mg/mL BSA) and vacuum filtration using a 24-well sampling manifold and Whatman GF/B glass-fiber filters that have been soaked in wash buffer at 4°C for 24 h. Each reaction tube is washed five times with a 4-mL aliquot of buffer. The filters are oven-dried for 60 min and then placed in 5 mL of scintillation fluid, and radioactivity is quantitated by liquid scintillation spectrometry. Specific binding is defined as the difference between the binding that occurs in the presence and absence of 1 μM concentrations of the corresponding unlabeled ligand and is 70 to 80% of the total binding.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Following a 1-week acclimation period, CB1 (+/+) and (?/?) mice are food-deprived, given an intraperitoneal injection of Org27569 (30 mg/kg), rimonabant (10 mg/kg; positive control), or vehicle at 23 h, and placed in a plastic cage with access to water. A premeasured amount (2.3-2.6 g) of sweet cereal or standard chow is placed in the test cage from 24 to 26h. All mice receive each treatment condition in a counterbalanced design, with at least 96 h between test days.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4393 mL 12.1966 mL 24.3932 mL 60.9830 mL
5 mM 0.4879 mL 2.4393 mL 4.8786 mL 12.1966 mL
10 mM 0.2439 mL 1.2197 mL 2.4393 mL 6.0983 mL
15 mM 0.1626 mL 0.8131 mL 1.6262 mL 4.0655 mL
20 mM 0.1220 mL 0.6098 mL 1.2197 mL 3.0492 mL
25 mM 0.0976 mL 0.4879 mL 0.9757 mL 2.4393 mL
30 mM 0.0813 mL 0.4066 mL 0.8131 mL 2.0328 mL
40 mM 0.0610 mL 0.3049 mL 0.6098 mL 1.5246 mL
50 mM 0.0488 mL 0.2439 mL 0.4879 mL 1.2197 mL
60 mM 0.0407 mL 0.2033 mL 0.4066 mL 1.0164 mL
80 mM 0.0305 mL 0.1525 mL 0.3049 mL 0.7623 mL
100 mM 0.0244 mL 0.1220 mL 0.2439 mL 0.6098 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Org 27569
目錄號：
HY-13288
需求量：